Glimepiride

Sulfonylurea (third-generation), Insulin secretagogue, Antihyperglycemic agent

Glimepiride

Amaryl

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Summary

Classes

Sulfonylurea (third-generation), Insulin secretagogue, Antihyperglycemic agent

Common uses

Type 2 diabetes mellitus▲0▼

Pharmacy

Starting dose

1-2 mg PO once daily with breakfast; titrate by glycemic response

Preparations

1 mg, 2 mg, 4 mg tablets

US FDA Max

8 mg/d

Pharmacology

Routes

Oral

Onset

1-2 hours

Duration

24 hours

Half-life

~5-9 hours (parent and active metabolites combined)

Bioavailability

~100% (oral; not significantly affected by food)

Pregnancy

Avoid; switch to insulin. Neonatal hypoglycemia reported.^{[citation needed]}

Legal status

Rx-only in US

Purported mechanism

Glimepiride closes pancreatic β-cell ATP-sensitive potassium channels at a distinct binding site on SUR1, producing membrane depolarization, calcium entry, and glucose-independent insulin release.▲0▼ Compared with glyburide, glimepiride has a more pancreas-specific binding profile with less impact on cardiac KATP channels (relevant in the ischemic preconditioning debate) and a lower hypoglycemia rate at equieffective doses. CYP2C9 substrate; PGx genotype affects clearance.